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Active ingredients
Dexlansoprazole
Release form
Capsules
Composition
Capsules with modified release, composition (1 capsule): active substance: dexlansoprazole - 60 mg; excipients: sugar krupka (sucrose 25–36.6 mg, corn starch 3.4–15 mg) from 500 to 710 microns - 40 mg; magnesium carbonate - 16 mg; sucrose - 39.52 mg; low substituted hyprolosis - 12 mg; hyprolosis - 0.48 mg; hypromellose 2910 - 10.5067 mg; talc - 27.5499 mg; titanium dioxide - 6,9933 mg; a dispersion of copolymer methacrylic acid (methacrylic acid - 3.2292 mg, ethyl acrylate - 3.0888 mg, sodium lauryl sulfate - 0.1638 mg, polysorbate 80 - 0.5382 mg) - 7.02 mg; macrogol 8000 - 0.7 mg; Polysorbate 80 - 0.32 mg; colloidal silicon dioxide - 0.13 mg; methacrylic acid and methyl methacrylate copolymer (1: 2) - 31.9 mg; methacrylic acid and methyl methacrylate copolymer (1: 1) - 10.64 mg; triethyl citrate - 4.24 mg; shell: carrageenan - 0.24–0.78 mg; potassium chloride - 0.18–0.6 mg; titanium dioxide - 2.52 mg; dye FD & C blue No2 aluminum varnish - 1.08 mg; iron dye black oxide - 0 mg; hypromellose - q.s. up to 48/60 mg; peeled gray ink for marking (iron dye red oxide, iron dye yellow oxide, dye FD & C blue No2 aluminum varnish, carnauba wax, shellac, glyceryl monooleate) - trace amounts
Pharmacological effect
anti-ulcer inhibiting proton pump
Pharmacokinetics
Suction; Dexansoprazole is well absorbed when taken orally. Its bioavailability is 76% or more. The two-component composition of the drug Dexilant determines the absorption in the form of two pH-dependent phases. The first peak of the concentration of the active substance occurs in the range from 1 to 2 hours after ingestion (1st phase release of the active substance) and the second in the interval from 4 to 5 hours (2nd phase release of the active substance), respectively. After 5 days of administration of dexlansoprazole in plasma dosages of 30 and 60 mg Cmax is 658 and 1397 ng / ml, respectively; AUC is 3275 ng · h / ml and 6529 ng · h / ml after 5 days of administration of dexlansoprazole in dosages of 30 and 60 mg, respectively; Distribution; The binding of dexlansoprazole to plasma proteins is 96.1–98.8%; Metabolism; Dexansoprazole is extensively metabolized in the liver to inactive metabolites as a result of oxidation, reduction, and subsequent formation of sulfate, glucuronide, and glutathione compounds .; The oxidation is carried out with the help of the cytochrome P450 enzyme system, which participates both in the hydroxylation process (mainly CYP2C19 isoenzyme) and in the oxidation process (CYP3A4 isoenzyme).CYP2C19 isoenzyme is a polymorphic hepatic isoenzyme that exists in 3 fractions that exhibit different properties in the metabolism of substrates: fast, moderate and slow metabolisers. Dexansoprazole is the main component in the blood plasma, regardless of the type of metabolizer according to the CYP2C19 isoenzyme. In the case of medium and strong metabolisers of the CYP2C19 isoenzyme, the main metabolite in the blood plasma is 5-hydroxydexanesoprazole and its glucuronic compound. In weak metabolisers of the isoenzyme CYP2C19 - dexlansoprazole sulfone .; Derivation; T1 / 2 of the drug - 1-2 hours; Clearance after 5 days of dexlansoprazole is 11.4 and 11.6 l / h for dosages of 30 and 60 mg, respectively; The drug is excreted through the kidneys (about 51%) and 48% is excreted through the intestine .; Since the drug is extensively metabolized in the liver, dose reduction is not required when using dexlansoprazole in patients with impaired renal function. As in patients with normal renal function, a change in pharmacokinetics is not expected.
Indications
treatment of erosive esophagitis of any severity; ; maintenance therapy after treatment of erosive esophagitis and relief of heartburn; symptomatic treatment of gastroesophageal reflux disease (GERD, including NERD - non-erosive reflux disease).
Contraindications
hypersensitivity to any of the components of the drug; ; combined use with HIV protease inhibitors, the absorption of which depends on the pH of the stomach (such as atazanavir, nelfinavir), due to a significant decrease in their bioavailability; ;pregnancy; ; lactation period; patients with hereditary fructose intolerance, glucose-galactose malabsorption, or sugar-isomalta insufficiency (the product contains sucrose); ; age up to 18 years old .; With care: taking tacrolimus at the same time; CYP2C19 isoenzyme inhibitors (such as fluvoxamine); warfarin (under the control of PF and INR); methotrexate.
Use during pregnancy and lactation
Before starting treatment with dexlansoprazole, the possibility of a malignant neoplasm of the gastrointestinal tract should be excluded, since the drug can mask the symptoms and delay the correct diagnosis .; If symptoms persist despite adequate treatment,then further investigation should be carried out .; When taking proton pump inhibitors, which include dexlansoprazole, increases the risk of gastrointestinal infections, accompanied by diarrhea, the causative agents of which are bacteria of the genus Clostridium difficile, especially in hospitalized patients. This should be taken into account if the patient’s condition does not improve in the treatment of diarrhea. Patients in this case are advised to take the minimum effective dose of dexlansoprazole with the shortest duration of treatment .; In patients receiving high doses of the drug or with prolonged therapy with proton pump inhibitors (PPI) for a year or more, the risk of osteoporotic fractures of the thighs, hands and spine increases. Patients at risk for osteoporotic fractures should adhere to the recommended dosages (see “
Dosage and administration
”) .; In rare cases, patients experienced symptomatic and asymptomatic hypomagnesaemia when taking drugs with IIT for at least 3 months, and in most cases, when taken for a year. Symptoms of hypomagnesemia are tetany, arrhythmia, and seizures. Treatment is the replenishment of magnesium and the discontinuation of taking drugs IDU. In patients who need long-term treatment or at the same time taking drugs IDU with digoxin or other drugs that can cause hypomagnesemia (such as diuretics), it is necessary to control the concentration of magnesium in the blood serum before and during treatment .; Impact on the ability to drive vehicles / mechanisms. Because of the likelihood of dizziness and visual impairment, you should refrain from driving and other mechanisms that require increased attention.Dosage and administration
Inside, the capsule is taken entirely regardless of the meal .; You can also open the capsule, pour the granules from it into a tablespoon and mix them with applesauce; then swallow immediately without chewing .; Treatment of erosive esophagitis of any severity. The recommended dose is 60 mg 1 time per day. The course of treatment is 8 weeks; Maintenance therapy after treatment of erosive esophagitis and relief of heartburn. The recommended dose is 30 mg 1 time per day.In the conducted studies, the course of treatment was up to 6 months; For patients with moderate and severe erosive esophagitis, the recommended dose is 60 mg 1 time per day. In the conducted studies, the course of treatment was up to 6 months; Symptomatic treatment of gastroesophageal reflux disease (GERD, including NERD - non-erosive reflux disease). The recommended dose is 30 mg 1 time per day. The course of treatment is 4 weeks; In patients with impaired liver function of moderate severity (Child-Pugh class B), the daily dose should not exceed 30 mg of dexlansoprazole. There are no clinical data on taking the drug in patients with severe disorders (Child-Pugh class C) .; Dose adjustment in elderly patients, patients with impaired renal function and with impaired liver function of mild severity (Child-Pugh class A) is not required.
Side effects
Dexansoprazole can be administered without the risk of drug interaction to patients taking clopidogrel. In the case of co-administration of a dose adjustment, clopidogrel is not required. The absence of clinically significant drug interactions with phenytoin, theophylline and diazepam is also noted .; The simultaneous use of dexlansoprazole may affect the absorption of drugs, the bioavailability of which depends on the pH of the stomach (for example, ampicillin esters, digoxin, iron salts, ketoconazole, erlotinib) .; Simultaneous administration with tacrolimus can lead to an increase in plasma tacrolimus concentration, especially in post-transplant patients who are moderate or slower metabolizers of the CYP2C19 isoenzyme .; When taken simultaneously with fluvoxamine, there is a possibility of an increase in systemic exposure to dexlansoprazole .; The simultaneous administration of dexlansoprazole and methotrexate can lead to an increase and maintenance of a high concentration of methotrexate and / or its serum metabolite, which, accordingly, can lead to the development of toxicity of methotrexate. If you need to receive high doses of methotrexate, it is recommended to temporarily discontinue dexlansoprazole.
Overdose
The most frequent (at least 2%) undesirable side reactions are diarrhea, flatulence, abdominal pain, nausea, vomiting,upper respiratory tract infection .; The following are data on unwanted adverse reactions depending on the frequency of their occurrence: very often - ≥ 1/10; often ≥1 / 100 and <1/10; infrequently - ≥1 / 1000 and <1/100; rarely, ≥1 / 10000 and <1/1000; very rarely - <1/10000, including individual cases; frequency unknown (cannot be estimated based on available data) .; On the part of the immune system: frequency is unknown - hypersensitivity (including anaphylactic reactions), malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis, exfoliative dermatitis, anaphylactic shock .; On the part of metabolism and nutrition: the frequency is unknown - hypomagnesaemia, hyponatremia .; On the part of the digestive tract: often - diarrhea, discomfort and pain in the abdomen, constipation, flatulence, nausea, vomiting; infrequently - dry mouth; rarely - oral candidiasis; frequency is unknown - swelling of the oral mucosa, pancreatitis .; On the part of the kidneys and urinary tract: the frequency is unknown - acute renal failure .; On the part of the liver and biliary tract: infrequently - changes in the indicators of the functional activity of the liver; frequency unknown - drug hepatitis .; On the part of the skin and subcutaneous tissues: infrequently - rash, hives, itching; frequency is unknown - leukocytoclastic vasculitis, generalized rash .; On the part of the respiratory system, organs of the chest and mediastinum: often - infectious diseases of the upper respiratory tract; infrequently - cough; frequency is unknown - swelling of the larynx, feeling of tightness in the throat .; On the part of the blood and lymphatic system: the frequency is unknown - autoimmune hemolytic anemia, idiopathic thrombocytopenic purpura .; On the part of the musculoskeletal and connective tissue: the frequency is unknown - fractures .; On the part of the vessels: infrequently - the attack of heat (tides), increased blood pressure .; From the nervous system: often - headache; infrequently - dizziness, dysgeusia; rarely - paresthesia, convulsions; frequency unknown - stroke, transient ischemic attack .; On the part of the organ of vision: rarely - visual impairment; frequency unknown - fog; On the part of the organ of hearing and labyrinth disorders: rarely - vertigo; frequency is unknown - decrease in hearing .; Mental Disorders: Infrequently - insomnia, depression; rarely - auditory hallucinations .; General disorders: infrequently - weakness, changes in appetite; frequency unknown - swelling of the face.
Interaction with other drugs
Precautionary measures
special instructions
There were no reports of significant cases of dexilant overdose.Repeated dose of 120 mg and a single dose of 300 mg did not cause serious side effects. A side effect was observed in the form of an increase in blood pressure above 140/90 mm Hg. while taking the drug Dexilant, 60 mg 2 times a day .; However, in the case of overdose, symptomatic therapy is carried out only in the presence of clinical manifestations .; Dexansoprazole is not excreted by hemodialysis.